Inhibition and induction of CYP enzymes in humans: an update
The cytochrome P450 (CYP) enzyme family is the most important enzyme system catalyzing
the phase 1 metabolism of pharmaceuticals and other xenobiotics such as herbal remedies …
the phase 1 metabolism of pharmaceuticals and other xenobiotics such as herbal remedies …
The PPARs: from orphan receptors to drug discovery
Dietary fat intake is an environmental factor that affects many aspects of human health. 1
Several lines of evidence suggest that common diseases of modern society are associated …
Several lines of evidence suggest that common diseases of modern society are associated …
Sequence diversity in CYP3A promoters and characterization of the genetic basis of polymorphic CYP3A5 expression
P Kuehl, J Zhang, Y Lin, J Lamba, M Assem… - Nature …, 2001 - nature.com
Variation in the CYP3A enzymes, which act in drug metabolism, influences circulating
steroid levels and responses to half of all oxidatively metabolized drugs. CYP3A activity is …
steroid levels and responses to half of all oxidatively metabolized drugs. CYP3A activity is …
A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis
B Goodwin, SA Jones, RR Price, MA Watson… - Molecular cell, 2000 - cell.com
Bile acids repress the transcription of cytochrome P450 7A1 (CYP7A1), which catalyzes the
rate-limiting step in bile acid biosynthesis. Although bile acids activate the farnesoid X …
rate-limiting step in bile acid biosynthesis. Although bile acids activate the farnesoid X …
Species differences between mouse, rat, dog, monkey and human CYP-mediated drug metabolism, inhibition and induction
M Martignoni, GMM Groothuis… - Expert opinion on drug …, 2006 - Taylor & Francis
Animal models are commonly used in the preclinical development of new drugs to predict
the metabolic behaviour of new compounds in humans. It is, however, important to realise …
the metabolic behaviour of new compounds in humans. It is, however, important to realise …
Induction of phase I, II and III drug metabolism/transport by xenobiotics
C Xu, CYT Li, ANT Kong - Archives of pharmacal research, 2005 - Springer
Drug metabolizing enzymes (DMEs) play central roles in the metabolism, elimination and
detoxification of xenobiotics and drugs introduced into the human body. Most of the tissues …
detoxification of xenobiotics and drugs introduced into the human body. Most of the tissues …
The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity
JL Staudinger, B Goodwin, SA Jones… - Proceedings of the …, 2001 - National Acad Sciences
The pregnane X receptor (PXR) is the molecular target for catatoxic steroids such as
pregnenolone 16α-carbonitrile (PCN), which induce cytochrome P450 3A (CYP3A) …
pregnenolone 16α-carbonitrile (PCN), which induce cytochrome P450 3A (CYP3A) …
Bile acid receptors as targets for drug development
The intracellular nuclear receptor farnesoid X receptor and the transmembrane G protein-
coupled receptor TGR5 respond to bile acids by activating transcriptional networks and/or …
coupled receptor TGR5 respond to bile acids by activating transcriptional networks and/or …
Cryptochromes: blue light receptors for plants and animals
Cryptochromes are blue, ultraviolet-A photoreceptors. They were first characterized for
Arabidopsis and are also found in ferns and algae; they appear to be ubiquitous in the plant …
Arabidopsis and are also found in ferns and algae; they appear to be ubiquitous in the plant …
Structure of a serpin–protease complex shows inhibition by deformation
The serpins have evolved to be the predominant family of serine-protease inhibitors in man,.
Their unique mechanism of inhibition involves a profound change in conformation, although …
Their unique mechanism of inhibition involves a profound change in conformation, although …